The pharmacokinetic properties of chloroquine are still under debate. To establish the pharmacokinetics of a single dose of chloroquine and its metabolites, 19 healthy volunteers, including one Black and one albino subject, received a single dose of chloroquine 600mg. In addition, one participant also received an oral dose of de-ethylchloroquine 150mg. Blood and saliva samples were obtained up to 77 days after drug administration. High-performance liquid chromatography was used to measure the concentrations of chloroquine, de-ethylchloroquine andbis-de-ethylchloroquine. The mean volume of distribution (Vd), elimination half-life (t½) and clearance (CL) of chloroquine were 411 L/kg, 432 hours and 0.77 L/h/kg, respectively. For de-ethylchloroquine these values were 161 L/kg, 649 hours and 0.18 L/h/kg. The results of the Black and albino subject were similar. When 150mg of this compound was administered, the Vd of deethylchloroquine was 122 L/kg, t½was 529 hours and CL was 0.16 L/h/kg.Bis-de-ethylchloroquine was detectable in 6 volunteers. No evidence for a bimodal distribution of chloroquine elimination was found in this study. Concentrations of chloroquine in saliva in the terminal elimination phase were 3-fold higher than in plasma.